Synthesis and Bioactivity Evaluation of Ethyl 1-Arylmethyl-3-aryl-1H-pyrazole-5-carboxylate Deriva-tives

Abstract

Ethyl 3-aryl-1H-pyrazole-5-carboxylate reacted with arylmethyl chloride in acetone or acetonitrile in the presence of potassium carbonate to afford 1-arylmethyl-3-aryl-1H-pyrazole-5-carboxylate derivatives in good yields. The substituent on aryl moiety and solvent can influence on the yields of the reactions. The structures of all products were confirmed by ¹H NMR, ¹³C NMR, IR and MS spectra. The structure of compound 3c was determined by X-ray single crystal diffraction method. The compounds 3a～3d promoted HUVEC apoptosis at the concentrations of 5～20 μmol•L^－1 to a certain extent and the effect on the cell viability was dose-dependent.

Key words: synthesis, characterization, apoptosis, vascular endothelial cell, pyrazole derivative

Cite this article

DING Xiao-Ling,b, MENG Ning^c, XIA Yong^a, WANG Li-Juan,d
ZHANG Xiao-Feng^a, ZHAO Bao-Xiang*^,a, MIAO Jun-Ying*^,c. Synthesis and Bioactivity Evaluation of Ethyl 1-Arylmethyl-3-aryl-1H-pyrazole-5-carboxylate Deriva-tives[J]. Chin. J. Org. Chem., 2007, 27(12): 1542-1546.

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